Modified release compositions for DPP-IV inhibitors

a technology of dppiv inhibitors and compositions, which is applied in the direction of peptide sources, extracellular fluid disorders, metabolic disorders, etc., can solve the problems of all three classes of compound having side effects, a major threat to the health of the citizens of the western world, and difficulty in controlling type i diabetes

Inactive Publication Date: 2007-05-03
F HOFFMANN LA ROCHE INC
View PDF47 Cites 18 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] In one embodiment of the present invention, provided is a pharmaceutical composition comprising a therapeutic...

Problems solved by technology

Control of Type I diabetes is difficult and requires exogenous insulin administration.
Type II diabetes is a condition that poses a major threat to the health of the citizens of the western world.
However, all three classes of compound have side effects.
The biguanides, for example metformin, are unspecific and in certain cases have been associated with lactic acidosis, and need to be given over a longer period of time, i.e. they are not suitabl...

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Modified release compositions for DPP-IV inhibitors
  • Modified release compositions for DPP-IV inhibitors
  • Modified release compositions for DPP-IV inhibitors

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0410] Coated tablets with the compositions shown in the table below are made according to standard procedures. The specific DPP-IV inhibitor mentioned in the table can be replaced by other DPP-IV inhibitors mentioned above.

Descrip-100 mg200 mg400 mgComponenttiontablettablettabletGranulate(2S)-1-{[2-DPPIV128.4mg256.8mg513.6mg(5-Methyl-2-inhibitorphenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrilemesylateMicrocrystallineFiller56.4mg112.80mg225.6mgCellulose(Avicel PH-101)Sodium stearylGlidant0.9625mg1.925mg3.85mgfumarateKernel(externel phase)TalcAnti-6mg9mg12mgadhesiveSodium stearylGlidant / 2mg3mg4mgfumarateLubricantCoatOpadryFilm9.50mg15.00mg30.00mgformerEudragit S 100Coat15mg25mg50mgTotal:217mg425mg850mg

example 2

[0411] Coated capsules with the compositions shown in the table below are made according to standard procedures. The specific DPP-IV inhibitor mentioned in the table can be replaced by other DPP-IV inhibitors mentioned above.

50 mg150 mgComponentDescriptioncapsulecapsuleGranulate(2S)-1-{[1,1-Dimethyl-DPP-IV50mg150mg3-(4-pyridin-3-yl-inhibitorimidazol-1-yl)-propylamino]-acetyl}-pyrrolidine-2-carbonitrileMicrocrystallineFiller56.4mg112.80mgCellulose(Avicel PH-102)Externel phaseTalcAnti-1.925mg3.85mgadhesiveSodium stearyl fumarateGlidant / 4.8125mg9.625mgLubricantCapsuleEudragit S:Eudragit25mg40mgL 25:75

example 3

[0412] Capsules with coated pellets with the compositions shown in the table below are made according to standard procedures. The specific DPP-IV inhibitor mentioned in the table can be replaced by other DPP-IV inhibitors mentioned above.

50 mg150 mgComponentDescriptioncapsulecapsuleGranulate(S)-1-((2S,3S,11bS)-2-DPP-IV50mg150mgAmino-9,10-dimethoxy-inhibitor1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4-fluoromethyl-pyrrolidin-2-oneMicrocrystallineFiller60mg80mgCellulose(Avicel PH-102)Pregelatinized starchBinder3050Externel phaseTalcAnti-1.925mg3.85mgadhesiveMagnesium stearateGlidant / 4.8125mg9.625mgLubricantCoatEudragit L:Eudragit60mg100mgFS 75:25Capsule

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Fractionaaaaaaaaaa
Fractionaaaaaaaaaa
Forceaaaaaaaaaa
Login to view more

Abstract

The present invention refers to pharmaceutical composition comprising a DPP-IV inhibitor.

Description

PRIORITY TO RELATED APPLICATIONS [0001] This application claims the benefit of European Application No. 05107393.0, filed Aug. 11, 2005, which is hereby incorporated by reference in its entirety. FIELD OF THE INVENTION [0002] The present invention relates to new pharmaceutical compositions comprising a DPP-IV inhibitor. [0003] All documents cited or relied upon below are expressly incorporated herein by reference. BACKGROUND [0004] The enzyme dipeptidyl peptidase IV (EC.3.4.14.5, abbreviated in the following as DPP-IV) is involved in the regulation of the activities of several hormones. In particular DPP-IV degrades efficiently and rapidly glucagon like peptide 1 (GLP-1), one of the most potent stimulators of insulin production and secretion. Inhibiting DPP-IV would potentiate the effect of endogenous GLP-1, leading to higher plasma insulin concentrations. In patients suffering from impaired glucose tolerance and type 2 diabetes mellitus, the resultant higher plasma insulin concentr...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K38/04A61K9/48A61K9/24
CPCA61K9/2027A61K9/209A61K9/4891A61K9/5026A61K31/00A61P3/10A61P3/08A61P43/00A61P5/48A61K9/20A61K9/50A61K9/48
Inventor LOEFFLER, BERND MICHAELMACDONALD, ALEXANDERROCHA, CYNTHIAWORTH, ERIC
Owner F HOFFMANN LA ROCHE INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap